C07D309/04

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

TRNA SYNTHETASE INHIBITORS
20230102879 · 2023-03-30 ·

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

TRNA SYNTHETASE INHIBITORS
20230102879 · 2023-03-30 ·

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

HETEROCYCLIC DERIVATIVES AS TRMP8 ANTAGONISTS

Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucosa.

HETEROCYCLIC DERIVATIVES AS TRMP8 ANTAGONISTS

Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucosa.

SSAO inhibitors and use thereof

The application relates to a compound of Formula (I′) or (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.

LIPOXYGENASE INHIBITORS
20230117592 · 2023-04-20 · ·

Various embodiments of the present disclosure are directed to compounds having Formula I, Formula II, Formula IIA, Formula III, Formula IIIA, Formula IIIB, and/or pharmaceutically acceptable salts thereof. The compounds can be suitable for inhibiting lipoxygenases and/or treating associated diseases. In some embodiments, subject compounds are used to prepare a composition that is effective in treating neurodegenerative diseases.

LIPOXYGENASE INHIBITORS
20230117592 · 2023-04-20 · ·

Various embodiments of the present disclosure are directed to compounds having Formula I, Formula II, Formula IIA, Formula III, Formula IIIA, Formula IIIB, and/or pharmaceutically acceptable salts thereof. The compounds can be suitable for inhibiting lipoxygenases and/or treating associated diseases. In some embodiments, subject compounds are used to prepare a composition that is effective in treating neurodegenerative diseases.

FERROPTOSIS INHIBITORS - DIARYLAMINE PARA-ACETAMIDES
20230159492 · 2023-05-25 · ·

Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.